Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDC00178

Target Information
NameProtein kinase C, theta type    
Type of targetClinical trial target    
SynonymsNPKC-theta    
Protein kinase C theta    
DiseaseImmune disease[1]
T cell leukemias
[ICD9: 208.9   ICD10: C91-C95]
[2]
Drug(s)Sotrastaurin acetatePhase IIhttp://clinicaltrials.gov/ct2/show/NCT01064791?term=Sotrastaurin&rank=1[3]
BioChemical ClassTransferases transferring phosphorus-containing groups    
EC NumberEC 2.7.1.-
PathwayAdipocytokine signaling pathway
T cell receptor signaling pathway
Tight junction
Vascular smooth muscle contraction
UniProt IDQ04759
PDB Structure1XJD; 2ENJ; 2ENN; 2ENZ; 2JED.    
FunctionThis is calcium-independent, phospholipid-dependent, serine- and threonine-specific enzyme.pkc is activated by diacylglycerol which in turn phosphorylates a range of cellular proteins. Pkc also serves as the receptor for phorbol esters.    
SequenceMSPFLRIGLSNFDCGSCQSCQGEAVNPYCAVLVKEYVESENGQMYIQKKPTMYPPWDSTF DAHINKGRVMQIIVKGKNVDLISETTVELYSLAERCRKNNGKTEIWLELKPQGRMLMNAR YFLEMSDTKDMNEFETEGFFALHQRRGAIKQAKVHHVKCHEFTATFFPQPTFCSVCHEFV WGLNKQGYQCRQCNAAIHKKCIDKVIAKCTGSAINSRETMFHKERFKIDMPHRFKVYNYK SPTFCEHCGTLLWGLARQGLKCDACGMNVHHRCQTKVANLCGINQKLMAEALAMIESTQQ ARCLRDTEQIFREGPVEIGLPCSIKNEARPPCLPTPGKREPQGISWESPLDEVDKMCHLP EPELNKERPSLQIKLKIEDFILHKMLGKGSFGKVFLAEFKKTNQFFAIKALKKDVVLMDD DVECTMVEKRVLSLAWEHPFLTHMFCTFQTKENLFFVMEYLNGGDLMYHIQSCHKFDLSR ATFYAAEIILGLQFLHSKGIVYRDLKLDNILLDKDGHIKIADFGMCKENMLGDAKTNTFC GTPDYIAPEILLGQKYNHSVDWWSFGVLLYEMLIGQSPFHGQDEEELFHSIRMDNPFYPR WLEKEAKDLLVKLFVREPEKRLGVRGDIRQHPLFREINWEELERKEIDPPFRPKVKSPFD CSNFDKEFLNEKPRLSFADRALINSMDQNMFRNFSFMNPGMERLIS
Target ValidationClick to Find Target Validation Information.    
Inhibitor2,3,3-Triphenyl-acrylonitrile[4]
2- (4-Hydroxy-phenyl)-3,3-diphenyl-acrylonitrile[4]
3,3-Bis- (4-hydroxy-phenyl)-2-phenyl-acrylonitrile[4]
3,3-Bis- (4-methoxy-phenyl)-2-phenyl-acrylonitrile[4]
3- (4-Hydroxy-phenyl)-2,3-diphenyl-acrylonitrile[4]
3- (4-Hydroxy-phenyl)-2,3-diphenyl-acrylonitrile[4]
4-HYDROXYTAMOXIFEN[4]
4-[1- (4-hydroxyphenyl)-3-methyl-1-butenyl]phenol[4]
4-cycloheptyliden (4-hydroxyphenyl)methylphenol[4]
4-cyclohexyliden (4-hydroxyphenyl)methylphenol[4]
Indolocarbazole analogue[5]
Indolocarbazole analogue[5]
Indolocarbazole analogue[5]
Indolocarbazole analogue[5]
Indolocarbazole analogue[5]
Indolocarbazole analogue[5]
Indolocarbazole analogue[5]
LY-317644[6]
LY-326449[7]
Phosphonoserine[8]
Phosphonothreonine[8]
RO-316233[9]
RO-320432[10]
Ro-32-0557[10]
Sotrastaurin acetate[3]
Staurosporine[8]
[2,2',   5',2'']Terthiophen-4-yl-methanol[11]
[2,2',   5',2'']Terthiophene-4,5''-dicarbaldehyde[11]
[2,2',   5',2'']Terthiophene-4-carbaldehyde[11]
MultitargetSotrastaurin acetate[3]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Protein kinase C-theta (PKCtheta): it's all about location, location, location. Immunol Rev. 2003 Apr;192:53-63. To Reference
Ref 2Protein kinase C-theta (PKCtheta), a potential drug target for therapeutic intervention with human T cell leukemias. Curr Cancer Drug Targets. 2002 Jun;2(2):125-37. To Reference
Ref 3Emerging drugs for psoriasis. Expert Opin Emerg Drugs. 2009 Mar;14(1):145-63. To Reference
Ref 4J Med Chem. 1992 Feb 7;35(3):573-83.Multivariate analysis by the minimum spanning tree method of the structural determinants of diphenylethylenes and triphenylacrylonitriles implicated in estrogen receptor binding, protein kinase C activity, and MCF7 cell proliferation. To Reference
Ref 5Bioorg Med Chem Lett. 2002 Jan 21;12(2):147-50.Mixed lineage kinase activity of indolocarbazole analogues. To Reference
Ref 6Bioorg. Med. Chem. Lett. 5(18):2093-2096 (1995) To Reference
Ref 7J Med Chem. 1996 Jul 5;39(14):2664-71.(S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta. To Reference
Ref 8Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 9J Med Chem. 1992 Jan;35(1):177-84.Inhibitors of protein kinase C. 1. 2,3-Bisarylmaleimides. To Reference
Ref 10Bioorg. Med. Chem. Lett. 4(11):1303-1308 (1994) To Reference
Ref 11Bioorg Med Chem Lett. 1999 Aug 2;9(15):2279-82.Novel protein kinase C inhibitors: synthesis and PKC inhibition of beta-substituted polythiophene derivatives. To Reference



 

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